| DC70518 |
IY7640 |
IY7640 (IY-7640) is a small molecule targeting the stalk region of the influenza HA protein, blocks HA-mediated membrane fusion of H1N1, H3N2, and influenza B viruses in cells.IY7640 demonstrated potency against H1N1, H3N2, H5N1, H7N9, and H9N2 subtypes of IAV, including the 2009 pandemic H1N1 (pH1N1) virus (A/Korea/01/2009, rK09), with EC50 of 0.62-220 uM in plaque reduction assay in MDCK cells.IY7640 successfully inhibited rK09 replication in cells at a level comparable to that of oseltamivir, K09 HA fusion was inhibited only by 1 uM IY7640.The stalk region of the influenza HA protein is highly conserved across different (sub)types of influenza viruses. |
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| DC70521 |
JCP276 |
JCP276 is a novel antibiotic and covalent inhibitor that disrupt M. tuberculosis growth by targeting multiple serine hydrolases.JCP276 is a narrow-spectrum inhibitor of Mycobacterium tuberculosis growth.JCP276 inhibits multiple nonessential serine hydrolases.JCP276 treatment caused accumulation of free lipids and a substantial decrease in lipooligosaccharides, linking SH inhibition to defects in cell envelope biogenesis. |
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| DC70522 |
JMN3-003 |
JMN3-003 is a host-directed inhibitor with potent antiviral activity against a panel of myxovirus family members with EC50 of 10-70 nM.JMN3-003 shows activity against MeV at 170 (viral CPE-reduction assay) and 30 nM (virus yield reduction assay) and does not display any detectable acute cytotoxicity.JMN3-003 also shows superb antiviral activity against a selection of clinical-relevant paramyxovirus (RSV, MuV, and HPIV3) and orthomyxovirus (influenza) family members. |
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| DC70530 |
JTP-0157602 |
JTP-0157602 (JTP0157602) is a novel non-catalytic site integrase inhibitor of HIV-1 integrase (IN), inhibits the interaction between LEDGF IBD and IN with IC50 of 4.2 nM.JTP-0157602 exhibits potent antiviral activity against HIV-1 with EC90 of 138 nM.JTP-0157602 retained potent antiviral activity (EC50=1-6 nM) against a broad panel of recombinant viruses with INSTI-related resistant mutations, including multiple substitutions that emerged in clinical studies of INSTIs (IN strand transfer inhibitors (INSTIs).JTP-0157602 inhibited HIV-1 replication mainly during the late-phase of the replication cycle.JTP-0157602 binds to the LEDGF/p75 binding pocket of HIV-1 integrase (IN). |
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| DC70543 |
KNI-1657 |
KNI-1657 (KNI1657) is a highly potent HIV-1 protease inhibitor (97% inhibition at 1 nM) with high sensitivity against lopinavir/ritonavir- or darunavir-resistant strains; inhibits wild-type HIV-1 (pNL4-3) and LPV-resistant strain A17 with IC50 of <3 and 25 nM, respectively. |
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| DC70555 |
KYT-1 |
KYT-1 is a potent, selective inhibitor of P. gingivalis virulence factor Arg-gingipain (Rgp) with Ki 40 nM (RgpA/B).KYT-1 showed significant inhibitory effects on SMC proliferation stimulated by Porphyromonas gingivalis. |
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| DC70556 |
KYT-36 |
KYT-36 is a potent, selective, and bioavailable inhibitor of P. gingivalis virulence factor gingipain K (Kgp, lysine-gingipain), potently and selectively inhibits Kgp with Ki of 0.27 nM, respectively.KYT-36 consists of benzyloxycarbonyl (BOC), L-glutaminyl (GLN), methylphenylamino (MPA), L-lysinyl (LYS), and benzylcarbamoyl (BCA) moieties.KYT-36 strongly inhibited degradation of host proteins in culture supernatants and abolished thriving of P. gingivalis in cell cultures and in periodontal pockets in vivo.KYT-36 prevented Kgp-triggered vascular permeability in guinea pigs, i.e. demonstrating its efficacy against bacterial virulence in vivo, with no toxicity effects. |
|
| DC70565 |
LFF-571 |
LFF571 is a semisynthetic thiopeptide and bactericidal antibiotic that interferes with bacterial protein synthesis by inhibition of elongation factor EF-Tu, LFF571 is potent in vitro activity against C.difficile strains with MIC90 of 0.25 ug/mL.LFF571 demonstrated activity against most other Gram-positive rods and cocci (MIC50/90, 0.125/0.25 μg/mL) except for bifidobacteria and some species of lactobacilli, showed reduced active activity against Gram-negative anaerobes with MICs for Bacteroides fragilis of 4 and 8 μg/mL.LFF571 inhibits exogenous protein synthesis elongation factor EF-Tu and interferes with the ability for EF-Tu to deliver aminoacylated tRNA to the ribosome. |
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| DC70570 |
LPXC-516 |
LPXC-516 is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC), potent against the P. aeruginosa isolates with MIC90 of 2 ug/mL. |
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| DC70585 |
MBX3132 |
MBX3132 is a small mocule inhibitor of AcrB multidrug efflux pump, fully potentiates the activity of a broad range of antibiotics at 0.1 uM; does not exhibit membrane-disrupting or antibacterial activity. |
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| DC70587 |
MCB-3681 |
MCB 3681 is a quinolonyl-oxazolidinone bactericidal antibiotic, has activity in vitro against Gram-positive bacteria. MCB3681 has a potent in vitro activity against C. difficile with MIC90 of 0.064 ug/ml. |
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| DC70591 |
mCLB073 |
mCLB073 (mCLB 073) is a more potent, specific, oral small molecule agonist of the Mtb adenylyl cyclase Rv1625c, an optimized analog of the V-59 for in vivo use.mCLB073 exhibited 17-fold potency improvement against Mtb in cholesterol media relative to V-59 while maintaining excellent pharmacokinetic properties and a good safety profile.mCLB073 (30 mg/kg, oral) reduced Mtb CFUs in the lungs of mice significantly and decreased the extent of lung pathology by 45%. |
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| DC70596 |
MGB-BP-3 |
MGB-BP-3 is a potent bactericidal antibiotic with a completely novel mode of action, selectively binds to the minor grove of microbial DNA, has the potential for Clostridioides difficile infection (CDI). |
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| DC70608 |
MMV019721 |
MMV019721 (MMV019721) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 73 nM.MMV019721 directly inhibits PfAcAS by preventing CoA binding.MMV019721 has activity against blood-stage parasites in vitro (P. falciparum 3D7, EC50=460 nM) and against liver-stage P. berghei parasites (Pbluc EC50=2,000 nM).MMV019721 directly and selectively inhibits PfAcAS activity in vitro. |
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| DC70609 |
MMV030084
Featured
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MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.MMV030084 is a promising Plasmodium PKG-targeting chemotype. |
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| DC70610 |
MMV084978 |
MMV084978 (MMV 084978) is an antiplasmodial drug-like compound tageting Plasmodium falciparum acetyl-coenzyme A synthetase (PfAcAS), directly and selectively inhibit PfAcAS activity in vitro with IC50 of 370 nM.MMV084978 directly inhibits PfAcAS by preventing CoA and acetate binding.MMV084978 demonstrated in vitro efficacy (P. falciparum Dd2 EC50=150 nM) with increased liver-stage potency (Pbluc EC50= 520 nM).MMV084978 directly and selectively inhibit PfAcAS activity in vitro. |
|
| DC70611 |
MMV675968 |
MMV675968 is a potent, small molecule inhibitor of Toxoplasma gondii (T. gondii) with IC50 of 0.02 uM, via the pathogen box.MMV675968 has been shown to be efficient against the planktonic form of C. albicans.MMV675968 showed an antiplasmodial activity against P. falciparum.MMV675968inhibited the growth of all four A. baumannii test strains with IC50 of 0.6-2.7 uM, IC90 of 0.7-3.9 uM, and MIC of 1.6-10 uM. |
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| DC70612 |
MMV688533 |
MMV688533 is a potent antimalarial compound that displays fast parasite clearance in vitro and is not cross-resistant with known antimalarials, MMV688533 is highly potent against multiple P. falciparum strains with IC50 values in low nanomolar range (P. falciparum 3D7, IC50=1.9 nM).MMV688533 also showed excellent ex vivo activity against asexual blood-stage parasites from fresh P. falciparum isolates (median IC50=1.3 nM, range=0.02 to 6.3 nM).MMV688533 remained potent in ex vivo assays against both P. falciparum and P. vivax with IC50 of 18.9 and 12.0 nM respectively.MMV688533 displayed fast and potent in vivo efficacy and favorable in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetic properties.MMV688533 antiplasmodial activity is unrelated to existing antimalarials and selects for low-grade resistance mediated in part by mutations in PfACG1 and PfEHD. |
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| DC70613 |
MMV688844 |
MMV688844 (MMV844) is a piperidine-4-carboxamide with bactericidal properties against M. abscessus, targets mycobacterial DNA gyrase. |
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| DC70626 |
Mtb CoaBC inhibitor 1f |
Mtb CoaBC inhibitor 1f is a direct small molecule inhibitor of Mtb 4'-phosphopantothenoyl-l-cysteine synthetase (PPCS, CoaB) domain of the bifunctional Mtb CoaBC (IC50=15.6 uM).Mtb CoaBC inhibitor 1f inhibit CoaBC uncompetitively with respect to 4'-phosphopantothenate, the substrate for the CoaB-catalyzed reaction.Mtb CoaBC inhibitor 1f inhibits Mtb growth in whole-cell activity against Mtb H37Rv (MIC=25.9 uM). |
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| DC70633 |
N205 |
N205 is a novel anti-malaria compound with in vitro IC50 of 1.3 nM against Plasmodium falciparum (3D7); demonstrates excellent rodent pharmacokinetic and in vivo antimalarial efficacy studies in the mouse Plasmodium berghei and Plasmodium falciparum Pf3D70087/N9 severe combined immunodeficiency (SCID) mouse models. |
|
| DC70640 |
NBD-14273 |
NBD-14273 is a CD4-mimetic, small-molecule HIV-1 entry inhibitor with IC50 of 0.13 uM.NBD-14273 showed both improved antiviral activity and selectivity index (SI) against HIV-1HXB2 compared to NBD-14136.NBD-14273 displayed potenct against a large panel of 50 HIV-1 Env-pseudotyped viruses representing clinical isolates of diverse subtypes. |
|
| DC70646 |
NEU-4438 |
NEU-4438 (NEU4438) is a potent inhibitor of P. falciparum with EC50 of 13 nM (T. brucei), demonstrates improved aqueous solubility (880 uM) compared to NEU-1953; reduced parasitemia 109 fold in trypanosome-infected mice. |
|
| DC70661 |
NPG9 |
NPG9 (NSR inhibitor NPG9) is a small molecule inhibitor of streptococcus agalactiaenisin resistance protein (NSR) with 58% inhibition at 100 uM (specific growth inhibition assay). |
|
| DC70681 |
PDE-I2 |
PDE-I2 is a potent and selective inhibitor of malaria proliferation with Pf IC50 of 18 nM.PDE-I2 is a precursor of the anticancer duocarmycin family that preserves the class's sequence-specific DNA binding but lacks its signature DNA alkylating cyclopropyl warhead.PDE-I2 retains comparable antimalarial potency to chloroquine.PDE-I2 is >1,000-fold less toxic to human cell lines than duocarmycin, with mitigated impacts on eukaryotic chromosome stability.PDE-I2 treatment induces severe defects in parasite nuclear segregation leading to impaired daughter cell formation during schizogony. |
|
| DC70717 |
PTC-672 |
PTC-672 (PTC672) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.4 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-672 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-672 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-672 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-672 showed 78% inhibition at 2.5 μM aginst Ng RNR activity, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.PTC-672 (30 mg/kg) demosntrates in vivo efficacy in a mouse model of gonorrhea. |
|
| DC70718 |
PTC-847 |
PTC-847 (PTC847) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.1 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-847 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-847 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-847 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-847 showed 93% inhibition aginst Ng RNR activity at 4 uM, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM. |
|
| DC70722 |
Q308
Featured
|
Q308 is a small molecule that silences the latent HIV-1 provirus by inhibiting Tat-mediated gene transcription and selectively downregulates the expression levels of the facilitated chromatin transcription (FACT) complex.Q308 induced the preferential apoptosis in HIV-1 latently infected cells, Q308 may reduce the size of the viral reservoir. |
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| DC70724 |
Quabodepistat |
Quabodepistat (OPC-167832) is a highly potent antituberculosis agent with MIC of 0.00024 to 0.002 ug/mL against Mycobacterium tuberculosis, targets DprE1 (IC50=258 nM, recombinant DprE1), an essential enzyme for cell wall biosynthesis.OPC-167832 showed MIC90 of 0.0048 and 0.0027 ug/mL against intracellular M. tuberculosis strains H37Rv and Kurono were 0.0048 and 0.0027, respectively.OPC-167832 showed potent bactericidal activities starting at a dose of 0.625 mg/kg of body weight in a mouse model of chronic TB.OPC-167832 exhibited significant combination effects in 2-drug combinations with delamanid, bedaquiline, or levofloxacin. |
|
| DC70725 |
QZN 34 |
QZN 34 is a small molecule pseudomonas aeruginosa PQS quorum-sensing system (PqsR) inhibitor with IC50 of 15 uM, kills planktonic Gram-positives (S. aureus, MIC 6.25 uM) but not Gram-negatives.QZN 34 prevented S. aureus biofilm formation, severely damaged established S. aureus biofilms, and perturbed P. aeruginosa biofilm development.QZN 34 killed planktonic Gram-positive pathogens including S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, and Clostridioides difficile but not Gram-negative bacteria such as P. aeruginosa and Escherichia. coli.QZN 34 eradicated the mixed-species biofilm against mixed S. aureus and P. aeruginosa biofilms when combined with aminoglycoside. |
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